中药挥发油具有独特的药性特征和理化性质，是一类性质优良的透皮促渗剂，但由于直接套用化学促渗剂研究思路，严重制约了中药挥发油透皮促渗剂的研究开发。在总结中药挥发油的研究进展及团队最新成果的基础上，基于四气和五味核心药性特征，提出和阐释了中药挥发油透皮促渗所蕴含的内在规律性及其机制，包括辛能开腠理、辛散温通、辛热能散能温3个层次的促渗规律，及辛味中药挥发油作用于角质层、辛温中药挥发油作用于局部血液循环、辛热中药挥发油倍半萜角质层贮库效应等促渗机制。并首次提出基于瞬时受体电位离子通道将促渗效果与四气药性相结合，建立“热者易效”核心机制假说。基于药性语言和现代机制总结了中药挥发油透皮促渗的规律与机制，为传统药性理论指导现代中药挥发油透皮促渗剂的研究开发提供科学依据。

Essential oils from traditional Chinese medicine (TCM) possess unique drug properties and physicochemical characteristics. Essential oils are regarded as a large class of excellent penetration enhancers (PEs). However, the research of essential oils as PEs has been seriously restricted because it has to comply with the current research design of chemical PEs. Based on the summary of the past research and the latest achievements of our team, the regularity and mechanism of penetration enhancement effect of essential oils from TCM are proposed and explained in detail according to drug property characteristics such as four natures and five flavors, which include three levels of promoting permeability, namely, “the pungent opening the skin barrier”, “the pungent and the warm property divergence and circulating” and “the pungent and the hot property divergence and warm” and the effect of pungent essential oils from TCM on stratum corneum, the effect of pungent and warm essential oils from TCM on topical blood circulation and the stratum corneum reservoir effect of sesquiterpenes of essential oils from TCM possessing both pungent and hot property. For the first time, it is proposed to combine the effect of promoting skin permeation based on transient receptor potential channels with the “four nature” properties, and to establish the core hypothesis of “hot property enhancing efficacy”. The present paper summarizes the regularity and mechanism of penetration enhancement effect of essential oils from TCM based on drug property language and modern mechanism, which can provide scientific basis for the research and development of TCM essential oil penetration enhancer guided by traditional drug property theory.

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国家自然科学基金资助项目(82173994);江苏省中药资源产业化过程协同创新中心重点项目(ZDXM-2020-25)